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Small lipidated anti-obesity compounds derived from neuromedin U.
Micewicz, Ewa D; Bahattab, Omar S O; Willars, Gary B; Waring, Alan J; Navab, Mohamad; Whitelegge, Julian P; McBride, William H; Ruchala, Piotr.
Afiliação
  • Micewicz ED; Department of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
  • Bahattab OS; Department of Cell Physiology and Pharmacology, University of Leicester, University Road, Leicester, LE1 9HN, UK.
  • Willars GB; Department of Cell Physiology and Pharmacology, University of Leicester, University Road, Leicester, LE1 9HN, UK.
  • Waring AJ; Department of Medicine, Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center, 1000 West Carson Street, Torrance, CA 90502, USA; Department of Physiology and Biophysics, University of California Irvine, 1001 Health Sciences Road, Irvine, CA 92697, USA.
  • Navab M; Department of Medicine, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
  • Whitelegge JP; Department of Psychiatry and Biobehavioral Sciences, University of California at Los Angeles, 760 Westwood Plaza, Los Angeles, CA 90024, USA; The Pasarow Mass Spectrometry Laboratory, The Jane and Terry Semel Institute for Neuroscience and Human Behavior, 760 Westwood Plaza, Los Angeles, CA 90024, U
  • McBride WH; Department of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.
  • Ruchala P; Department of Psychiatry and Biobehavioral Sciences, University of California at Los Angeles, 760 Westwood Plaza, Los Angeles, CA 90024, USA; The Pasarow Mass Spectrometry Laboratory, The Jane and Terry Semel Institute for Neuroscience and Human Behavior, 760 Westwood Plaza, Los Angeles, CA 90024, U
Eur J Med Chem ; 101: 616-26, 2015 Aug 28.
Article em En | MEDLINE | ID: mdl-26204509
ABSTRACT
A small library of truncated/lipid-conjugated neuromedin U (NmU) analogs was synthesized and tested in vitro using an intracellular calcium signaling assay. The selected, most active analogs were then tested in vivo, and showed potent anorexigenic effects in a diet-induced obese (DIO) mouse model. The most promising compound, NM4-C16 was effective in a once-weekly-dose regimen. Collectively, our findings suggest that short, lipidated analogs of NmU are suitable leads for the development of novel anti-obesity therapeutics.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neuropeptídeos / Fármacos Antiobesidade / Bibliotecas de Moléculas Pequenas / Obesidade Tipo de estudo: Prognostic_studies Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neuropeptídeos / Fármacos Antiobesidade / Bibliotecas de Moléculas Pequenas / Obesidade Tipo de estudo: Prognostic_studies Limite: Animals / Humans / Male Idioma: En Ano de publicação: 2015 Tipo de documento: Article